1,6-naphthyridine anti-convulsants

Details 1,6-naphthyridine anti-convulsants 1,6-naphthyridine anti-convulsants

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/435 (2006.01)

Patent

CA 2291254

Compounds of formula (I) and pharmaceutically acceptable salts thereof, where R1 is hydrogen, C1-6 alkyl optionally substituted by hydroxy or C1-4 alkoxy, or C1-6 alkylphenyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, C1-6 alkylO-, C1-6 alkylS-, C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkyl-, C1-6 alkenyl, C1-6 alkynyl, CF3, CF3O, CF3CO-, C1- 6 alkylCO-, C3-6 cycloaklylCO-, C3-6 cycloalkyl-C1-4 alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4 alkyl-, or -NR3R4 where R3 is hydrogen or C1-4 alkyl, and R4 is hydrogen, C1-4 alkyl, -CHO, -CO2C1-4 alkyl or -COC1-4 alkyl; or two R2 groups form a saturated carbocyclic ring optionally interrupted by oxygen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy; are useful in the treatment and prophylaxis of disorders treatable by anti-convulsants, e.g. epilepsy.

Composés représentés par la formule (I) et leurs sels acceptables sur le plan pharmaceutique, dans laquelle R?1¿ représente hydrogène, alkyle C¿1?-C¿6? éventuellement substitué par hydroxy ou alkoxy C¿1?-C¿4?, ou alkylphényle C¿1?-C¿6?; R?2¿ représente hydrogène ou trois substituants maximum sélectionnés dans halogène, NO¿2?, CN, N¿3?, alkyle O C¿1?-C¿6?, alkyle S C¿1?-C¿6?, alkyle C¿1?-C¿6?, cycloalkyle C¿3?-C¿6?, cycloalkyle C¿3?-C¿6?-alkyle C¿1?-C¿4?, alkényle C¿1?-C¿6?, alkynyle C¿1?-C¿6?, CF¿3?, CF¿3?O, CF¿3?CO-, alkyle C¿1?-C¿6? CO-, cycloalkyle C¿3?-C¿6? CO-, cycloalkyle C¿3?-C¿6?-alkyle C¿1?-C¿4? CO-, phényle, phénoxy, benzyloxy, benzoyle, phényle alkyle C¿1?-C¿4?-, ou -NR?3¿R?4¿ dans laquelle R?3¿ représente hydrogène ou alkyle C¿1?-C¿4? et R?4¿ représente hydrogène, alkyle C¿1?-C¿4?, -CHO, -CO¿2? alkyle C¿1?-C¿4? ou -CO alkyle C¿1?-C¿4?; ou deux groupes R?2¿ constituent un noyau carbocyclique saturé éventuellement interrompu par oxygène; X est sélectionné dans hydrogène, halogène, cyano, alkyle et alkoxy. Ces composés sont utiles pour le traitement et la prophylaxie de maladies pouvant être traitées par des anti-convulsifs, telles que l'épilepsie.

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